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Star polymer as well as preparation method and application thereof

A star-shaped polymer and reaction technology, which is applied in the field of biomedicine to achieve the effects of less variety, low price and easy regulation

Active Publication Date: 2018-11-13
CHINA AGRI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] However, it is difficult for the various nucleic acid carrier molecules that have been disclosed so far to have both high delivery efficiency and economical synthesis cost

Method used

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  • Star polymer as well as preparation method and application thereof
  • Star polymer as well as preparation method and application thereof
  • Star polymer as well as preparation method and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0078] This embodiment provides a star-shaped polymer and a preparation method thereof, the preparation method comprising:

[0079] (1) Preparation of star initiator

[0080] Dissolve 0.18mmol of pentaerythritol and 1.11mmol of triethylamine in dry tetrahydrofuran, and add 1.11mmol of 2-bromoisobutyryl bromide to the tetrahydrofuran solution dropwise at a rate of 60 drops per minute under nitrogen protection at 0°C. . After the dropwise addition was completed, it was stirred at 25°C for 48h. After the reaction, tetrahydrofuran was removed with a rotary evaporator, and the resulting mixture was dissolved in ethyl acetate, and then washed three times with saturated aqueous sodium carbonate solution and deionized water. The organic phase was dried with anhydrous sodium sulfate, and crystallized in glacial ether after rotary evaporation to obtain 50 mg of a white crystalline pure product, which was the star initiator, with a yield of 40%. The nuclear magnetic spectrum of the ch...

Embodiment 2

[0088] This embodiment provides a star-shaped polymer and a preparation method thereof, the preparation method comprising:

[0089] (1) Preparation of star initiator

[0090] The star initiator can be prepared by the same method as in Example 1.

[0091] (2) Reaction of star initiator with nitrogen-containing acrylate monomer

[0092] 0.055 mmol of initiator and 22 mmol of monomeric dimethylaminoethyl methacrylate (DMAEMA) were dissolved in 8 mL of dry tetrahydrofuran, and 3-4 freeze-pump cycles were performed. Under the protection of nitrogen, add 0.22mmol of cuprous bromide and 0.44mmol of N,N,N',N,'N"-pentamethyldiethylenetriamine, and react at 60°C for 7h after freezing again After the reaction, precipitated three times in diethyl ether, and vacuum-dried the obtained solid to constant weight to obtain about 2.4 g of white polymer P2 with a yield of 40%.

[0093] The chemical structural formula of gained star polymer P2 is:

[0094]

[0095] The NMR spectrum of the c...

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Abstract

The invention provides a star polymer as well as a preparation method and application thereof. The preparation method of the star polymer comprises the following steps: S1, mixing pentaerythritol with2-bromoisobutyryl bromide to obtain a star initiator; S2, carrying out mixed reaction on the star initiator with a nitrogenous acrylate monomer. Compared with exogenous nucleic acid with high preparation cost or nucleic acid molecules with low delivery efficiency, the star polymer provided by the invention has good water solubility and low cytotoxicity; the preparation method of the star polymeris simple and the preparation cost is low; the star polymer and exogenous nucleic acid molecules can form a stable compound which quickly enters cells.

Description

technical field [0001] The present invention relates to biomedicine, more specifically, to a star polymer and its preparation method and application. Background technique [0002] The biological cell membrane is mainly an elastic semipermeable membrane composed of protein, with a thickness of 8-10nm, and the outside is close to the cell wall. Its main function is to selectively exchange substances, absorb nutrients, discharge metabolic waste, secrete and transport proteins. [0003] The cell membrane of organisms is a natural barrier, and it is difficult for exogenous nucleic acid molecules, including DNA and RNA molecules, to penetrate the barrier of the cell membrane and enter the cell to play a role. In the fields of cell transfection, gene therapy, and transgenic applications, when introducing exogenous nucleic acid molecules into cells, including genetically engineered plasmids, special chemical reagents or equipment are required to create cell membrane gaps or use Agr...

Claims

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Application Information

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IPC IPC(8): C08F297/00C12N15/87C12N15/85
Inventor 沈杰黎剑浩郑洋尹梅贞
Owner CHINA AGRI UNIV
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